Chemical Property of Delamanid
Chemical Property:
- Appearance/Colour:White to brown solid
- Melting Point:195-196℃
- Boiling Point:653.7±65.0 °C(Predicted)
- PKA:3.99±0.20(Predicted)
- PSA：103.80000
- Density:1.45
- LogP:5.55600
- Storage Temp.:Hygroscopic, -20°C Freezer, Under inert atmosphere
- Solubility.:Chloroform (Sparingly), Ethyl Acetate (Slightly, Sonicated)
- XLogP3:5.6
- Hydrogen Bond Donor Count:0
- Hydrogen Bond Acceptor Count:11
- Rotatable Bond Count:7
- Exact Mass:534.17261902
- Heavy Atom Count:38
- Complexity:795
- Purity/Quality:
-
99%, *data from raw suppliers
Delamanid *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CC1(CN2C=C(N=C2O1)[N+](=O)[O-])COC3=CC=C(C=C3)N4CCC(CC4)OC5=CC=C(C=C5)OC(F)(F)F
- Isomeric SMILES:C[C@@]1(CN2C=C(N=C2O1)[N+](=O)[O-])COC3=CC=C(C=C3)N4CCC(CC4)OC5=CC=C(C=C5)OC(F)(F)F
- Recent ClinicalTrials:Protecting Households On Exposure to Newly Diagnosed Index Multidrug-Resistant Tuberculosis Patients
- Recent EU Clinical Trials:A Phase 3, Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel Group
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Description
Marketed by Otsuka, delamanid was approved in both the European
Union and Japan in 2014 as part of combination therapies for
multi-drug resistant tuberculosis (TB). Because delamanid exhibited
no adverse drug–drug interactions, it has found utility as a
combination therapy with standard antiretroviral drugs indicated
for TB. Delamanid blocks mycolic acid biosynthesis in Mycobacterium
tuberculosis, which allows its cell wall to be penetrated by
small molecule antivirals.
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Uses
Delamanid is a novel anti-tuberculosis medication that inhibits mycolic acid synthesis and shows potent in vitro and in vivo activity against drug-resistant strains of Mycobacterium tuberculosis.
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Clinical Use
Treatment of multi-drug resistant tuberculosis
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Drug interactions
Potentially hazardous interactions with other drugsAnalgesics: increased risk of ventricular arrhythmias
with methadoneAnti-arrhythmics: increased risk of ventricular
arrhythmias with amiodarone and disopyramideAntibacterials: possible increased risk of ventricular
arrhythmias with clarithromycin, erythromycin
and moxifloxacin; increased risk of ventricular
arrhythmias with pentamidine; concentration
reduced by rifampicinAntidepressants: possible increased risk of
ventricular arrhythmias with tricyclics.Antiepileptics: avoid with carbamazepine.Antipsychotics: increased risk of ventricular
arrhythmias with droperidol, haloperidol,
phenothiazines that prolong the QT interval and
pimozide.Antivirals: increased risk of ventricular arrhythmias
with saquinavirBeta-blockers: increased risk of ventricular
arrhythmias with sotalol.Cytotoxics: increased risk of ventricular arrhythmias
with arsenic trioxide and possibly vinblastine,
vincristine, vindesine, vinflunine and vinorelbineDomperidone: possible increased risk of ventricular
arrhythmias.
